ArticleBritish journal of pharmacology2001
In vivo evidence that protease-activated receptors 1 and 2 modulate gastrointestinal transit in the mouse.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 75 citations in OpenAlex.
- CharacterizingInternational journal of molecular sciences · 2025Article
- Altered functional responses by PAR1 agonist in murine dextran sodium sulphate-treated colon.Scientific reports · 2022Article
- Novel role of zonulin in the pathophysiology of gastro-duodenal transit: a clinical and translational study.Scientific reports · 2021Article
- Interleukin-10 and Zonulin Are Associated With Postoperative Delayed Gastric Emptying in Critically Ill Surgical Pediatric Patients: A Prospective Pilot Study.JPEN. Journal of parenteral and enteral nutrition · 2020Article
- The functional role of protease-activated receptors on contractile responses by activation of CaAmerican journal of physiology. Gastrointestinal and liver physiology · 2018Article
- Article
- Targeting proteinase-activated receptors: therapeutic potential and challenges.Nature reviews. Drug discovery · 2012Review
- The expression of protease-activated receptor 2 and 4 in the colon of irritable bowel syndrome patients.Digestive diseases and sciences · 2012Article
- Role of enteric nerves in immune-mediated changes in protease-activated receptor 2 effects on gut function.Neurogastroenterology and motility · 2010Article
- Gastrointestinal roles for proteinase-activated receptors in health and disease.British journal of pharmacology · 2008Review
- Proteinases and signalling: pathophysiological and therapeutic implications via PARs and more.British journal of pharmacology · 2008Review
- Role for protease activity in visceral pain in irritable bowel syndrome.The Journal of clinical investigation · 2007Article
- Recent insights into digestive motility in functional dyspepsia.Journal of gastroenterology · 2006Review
- Suppression of pancreatitis-related allodynia/hyperalgesia by proteinase-activated receptor-2 in mice.British journal of pharmacology · 2006Article
- Immune regulation of protease-activated receptor-1 expression in murine small intestine during Nippostrongylus brasiliensis infection.Journal of immunology (Baltimore, Md. : 1950) · 2005Article
- Review
- 2-Furoyl-LIGRL-NH2, a potent agonist for proteinase-activated receptor-2, as a gastric mucosal cytoprotective agent in mice.British journal of pharmacology · 2005Article
- Modulation of visceral pain and inflammation by protease-activated receptors.British journal of pharmacology · 2004Review
- Evidence for the presence of functional protease activated receptor 4 (PAR4) in the rat colon.Gut · 2004Article
- Involvement of EDHF in the hypotension and increased gastric mucosal blood flow caused by PAR-2 activation in rats.British journal of pharmacology · 2003Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Protease-activated receptors (PARs) 1 and 2 modulate the gastric and intestinal smooth muscle motility in vitro. In the present study, we examined if activation of PAR-2 and PAR-1 could alter gastrointestinal transit in mice. 2. Intraperitoneal administration of the PAR-2-activating peptide SLIGRL-NH(2), but not the inactive control LSIGRL-NH(2), at 1 - 5 micromol kg(-1), in combination with the aminopeptidase inhibitor amastatin at 2.5 micromol kg(-1), facilitated gastrointestinal transit in a dose-dependent manner. The human PAR-1-derived peptide SFLLR-NH(2) and the specific PAR-1 agonist TFLLR-NH(2), but not the inactive control FSLLR-NH(2), at 2.5 - 10 micromol kg(-1), in combination with amastatin, also promoted gastrointestinal transit. 3. The Ca2+-activated, small conductance K+ channel inhibitor apamin at 0.01 micromol kg(-1) significantly potentiated the actions of SLIGRL-NH(2) and TFLLR-NH(2) at subeffective doses. 4. The increased gastrointestinal transit exerted by either SLIGRL-NH(2) at 5 micromol kg(-1) or TFLLR-NH(2) at 10 micromol kg(-1) was completely abolished by the L-type Ca2+ channel inhibitor verapamil at 61.6 micromol kg(-1). In contrast, the tyrosine kinase inhibitor genistein at 18.5 micromol kg(-1) failed to modify the effects of the agonists for PAR-2 or PAR-1. 5. These findings demonstrate that PAR-1 and PAR-2 modulate gastrointestinal transit in mice in vivo. Our data also suggest that the PAR-1-and PAR-2-mediated effects are modulated by apamin-sensitive K+ channels and are dependent on activation of L-type Ca2+ channels, but independent of tyrosine kinase. Our study thus provides novel evidence for the physiological and/or pathophysiological roles of PARs 1 and 2 in the digestive systems, most probably during inflammation.
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